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The anti-inflammatory activity of two extracts from the aerial parts of Ledum palustre has been reported. The volatile oil was obtained by supercritical fluid extraction (SFE) and the essential oil by hydrodistillation (HD). The oils were analysed by gas chromatography-mass spectrometry to monitor their composition. Both extracts shared as main compound (41.0-43.4%) ledol (23.3-26.7%) and ascaridole (15.1-4.5%). The anti-inflammatory activity was evaluated by the subcutaneous carrageenan injection-induced hind paw oedema. The treated animals received essential oil (SFE and HD), the reference group received ketoprofen or piroxicam and the control group received NaCl 0.9%. A statistical analysis was performed by the Student t-test. The results show that L. palustre essential oil enhanced a significant inhibition of oedema (50-73%) for HD oil and (52-80%) for SFE oil. These results were similar to those obtained with piroxicam (70%) and ketoprofen (55%).
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Postoperative pain is an important parameter in discharge and rehabilitation in daycase arthroscopic knee surgery. This study compared the efficacy of intraarticular application of lornoxicam, bupivacaine and placebo on postoperative pain after arthroscopic knee surgery. With the approval of the local ethics committee and informed consent of the patients, 90 patients (ASA score I-II), aged between 18-65 years undergoing arthroscopic meniscectomy were included in this randomized, blinded, prospective study and were divided into three groups (30 patients each): 8 mg lornoxicam was applied to Group L (GL), 50 mg bupivacaine to Group B (GB) and normal saline to Group S (GS) in 20 mL volume intraarticularly. Postoperative analgesia was maintained by intravenous tramadol-HCl 50 mg/h at the first 4 h and then paracetamol 500 mg plus codeine 7.5 mg preparation as needed. The numeric rating scale (NRS) values were evaluated at rest and at active-passive motion at 4, 12, 24 and 48 h, total analgesic consumption were recorded. There were statistically significant differences between GS and GL and GS and GB in term of tramadol consumption (p < 0.05 and p < 0.05). The analgesiconsumption of GL patients at the end of 48 h were lower than GB and GS (p < 0.001 and p < 0.05). The NRS values of GL were always lower than the other groups with statistical significance at certain times. We concluded that intraarticular lornoxicam provided better pain control than bupivacaine and saline in arthroscopic knee surgery.
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The method showed a good linearity in the range of 2.5 division by 15.0 microg/mL (the correlation coefficient r = 0.9996). The detection limit (LD) was 0.44 microg/mL and the quantification limit (LQ) was 1.47 microg/mL. There were established the precision (RSD = 1.82%) and the accuracy (mean recovery is 100.79% in 97.55 division by BY 04.41% the range).
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We report a case of a transient corneal edema related to systemic NSAID treatment.
The pharmacokinetics of isoxicam 200 mg administered orally in 10 healthy male volunteers was studied before and during administration of acetylsalicylic acid 3.9 g daily by mouth starting 5 days after isoxicam. There was a statistically significant decrease in plasma isoxicam concentrations, but no significant change in time to reach maximum plasma concentration or disappearance time. The mechanisms of this interaction is probably competitive displacement of isoxicam from albumin by acetylsalicylic acid or salicylate. These results are consistent with the known effect of ASA in producing competitive displacement of other protein bound antiinflammatory drugs.
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Piroxicam is a poorly soluble NSAID, whose solubility is enhanced when included into beta-cyclodextrin. The preparation of a piroxicam-beta-cyclodextrin inclusion compound using supercritical CO2 was investigated.
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From a Mexican institutional perspective and probably in other Social Security Institutions in similar developing countries, the most cost-effective option for treatment of knee and/or hip OA would be celecoxib.
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Signs and symptoms of secondary overactive bladder (OAB) are observed both in course of infravesical obstruction of urine outflow in patients with benign prostatic hyperplasia, and as a result of development of hemorrhagic cystitis (HC) following administration of cyclophosphamide (CP). Non-steroidal antiinflammatory drugs (NSAIDs) alleviate symptoms of bladder overactivity reducing local synthesis of prostaglandins (PGs), but precise effects of those agents on functions of the autonomic nervous system (ANS) in course of OAB remain unknown. The purpose of this study was to evaluate the effect of piroxicam-induced prostaglandins (PGs) synthesis block on activity of the ANS in two experimental models of secondary OAB: bladder outlet obstruction (BOO) and cyclophosphamide-induced HC (CP-HC), by heart rate variability analysis (HRV). The experiment was performed on a group of rats with surgically induced 2-week BOO, and on a group of rats that were administered CP five times, with corresponding control groups. Study animals were given piroxicam (PRX) i.p. in two doses: 2 and 10 mg/kg b.w. In the BOO model, PRX in both doses revealed a trend for reduction of value of all non-normalized components of HRV. The lower PRX dose caused an increased nHF value, and PRX administered in the dose of 10 mg/kg b.w. caused an increase of the nLF value. In the CP-HC model, the lower PRX dose caused a trend for an increase of values of all non-normalized components, and the higher dose--for their decrease. Both doses of PRX in that model caused increase of the nLF value. Inhibition of PGs synthesis caused changes of ANS function in both models of OAB. Both in BOO and in CP-HC, PGs seem to be ANS-activating factors, responsible for maintenance of a high parasympathetic activity. In both models, inhibition of PGs synthesis with PRX administered at the dose of 10 mg/kg b.w. lead to functional reconstruction of ANS, with marked sympathetic predominance. That may contribute to reduction of the bladder contractile action and improvement of its compliance in the filling period, which was demonstrated by other authors in urodynamic tests for NSAIDs.
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Ionotropic gelation was used to entrap piroxicam into alginate and algino-pectinate mucoadhesive microspheres as a potential drug carrier for oral delivery of piroxicam. Microparticles with different drug to polymers ratio were prepared and characterized by encapsulation efficiency, particle size, DSC (differential scanning calorimetric), mucoadhesive property, gastroretentive time and drug release studies.
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The disk IDR values spanned six orders of magnitude (0.00014 to 114 mg min(-1) cm(-2)). The comparison of the miniaturized disk IDR values to published results using traditional dissolution bath apparatus indicated r (2) = 0.99.
All the F.A.N.S. used (Cinnoxicam, Salicylic Acetyl Acid) had an inhibitory effect on motility, as did L. Carnitine at high doses. We thought it interesting to observe if L. Carnitine added to the seminal fluid before F.A.N.S. blocked their effects.
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To compare the analgesic efficiency and adverse effects of postoperative patient-controlled intravenous analgesia (PCIA) with lornoxicam and sufentanil in patients undergoing oral maxillofacial surgery.
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The crystal structures of the two polymorphs were established by the experimental XRPD patterns. Form I was demonstrated to be triclinic with two kinds of intermolecular hydrogen bonds, while form II was orthorhombic with two kinds of intramolecular hydrogen bonds. The morphologies of form I and form II were observed to be rectangle and approximately oval, respectively.
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This study was designed to determine the effect of Mangifera indica flowers decoction, on the acute and subacute models of induced ulcer in mice and rats. A single oral administration of the aqueous decoction (AD) from M. indica up to a dose of 5 g/kg, p.o. did not produce any signs or symptom of toxicity in the treated animals. The oral pre-treatment with AD (250, 500 and 1000 mg/kg) in rats with gastric lesions induced by ethanol, decreased the gastric lesions from 89.0+/-6.71 (control group) to 9.25+/-2.75, 4.50+/-3.30 and 0, respectively. Pretreatment with AD (250, 500 and 1000 mg/kg) to mice with HCl/ethanol- or stress-induced gastric lesions resulted in a dose-dependent significant decrease of lesion index. In the piroxicam-induced gastric lesions, the gastroprotective effect of AD was reducing with the increase of the AD dose. In the pylorus-ligature, AD (p.o.) significantly decreased the acid output indicating the antisecretory property involved in the gastroprotective effect of M. indica. Treatment with AD during 14 consecutive days significantly accelerated the healing process in subacute gastric ulcer induced by acetic acid in rats. Pretreatment with N-nitro-l-arginine methyl ester (l-NAME), an inhibitor of NO-synthase, did not abolish the gastroprotective effects (99% with saline versus 80% with l-NAME) of AD against ethanol-induced gastric lesions. Pretreatment with N-ethylmaleimide (NEM), a blocker of endogenous sulphydryl group, significantly abolished the protective effects of AD against ethanol-induced gastric ulcers (95% with saline versus 47% with NEM). Phytochemical screening showed the presence of steroids, triterpenes, phenolic compounds and flavonoids. Estimation of the global polyphenol content in the AD was performed by Folin-Ciocalteu method and showed approximately 53% of total phenolic on this extract. These findings indicate the potential gastroprotective and ulcer-healing properties of aqueous decoction of M. indica flowers and further support its popular use in gastrointestinal disorders in Caribbean.
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Preoperative prophylactic and short term postoperative treatment with piroxicam was evaluated against placebo in 332 patients who were suspected of having a meniscal tear. 244 had undergone arthroscopic meniscal resection and 88 diagnostic arthroscopy only. The patients received 40 mg piroxicam preoperatively, 40 mg on the day of surgery and 20 mg on days 1 and 2. The patients who received piroxicam had significantly less pain and less swelling, independent of surgical procedure. After meniscal resection the patients achieved better range of motion and had less need of rescue analgesics. After diagnostic arthroscopy the patients returned to work sooner when treated with piroxicam. Adverse events were few in both groups and could not be related to medication. The study supports data recommending short term treatment with a non-steroid anti-inflammatory drug in arthroscopic procedures.
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Silica nanoparticles can be potentially considered the carriers of controlled drug systems. In this research, non-steroidal anti-inflammatory drugs were used. Diclofenac sodium and piroxicam were loaded on the considered nanosilica using solvent evaporation method. To prove drug encapsulation on the nanosilica and its rate, infrared spectroscopy, X-ray diffraction, and BET were used, and after proving the existence of the drug in the nanosilica matrix and determining the amount of loading, dissolution test was performed in an environment similar to that of stomach and intestine in terms of pH. Drug loading percentage showed that over 90% of drugs were loaded on nanosilica. Dissolution tests in stomach pH environment showed the control samples (drug without SBA-15) released considerable amount of drugs (about 90%) within first 15 min, when it was about 10-20% for the matrixes. Furthermore, release rate of drugs from matrixes has shown slower rate in comparison with control samples. It was indicated nanosilica has the ability of retaining the drugs in acidic pH and prevented their release. Furthermore, the drugs were released in a controlled manner in small intestine, which is the main absorption site.
Piroxicam, a nonsteroidal antiinflammatory drug, was given to 62 dogs bearing naturally occurring tumors in a phase I clinical trial. Dose escalation was performed, with oral doses ranging from 0.5 mg/kg every 48 h (q48h) to 1.5 mg/kg q48h being tested. Dose-limiting gastrointestinal irritation/ulceration occurred in all four animals that received 1.5 mg/kg q48h. The maximum tolerated dose was 1 mg/kg q48h. Subclinical renal papillary necrosis occurred in two dogs (initial dosages, 1 and 1.5 mg/kg q48h, respectively). Following dose escalation, an additional group of dogs was treated with 0.3 mg/kg piroxicam q24h per os, the accepted canine dosage prior to this trial. Inclusion of this treatment group enabled evaluation of the toxicity of and tumor response to a daily dosage regimen. No complete remissions occurred in this trial. Partial remission was documented in three of ten dogs exhibiting transitional-cell carcinoma, in three of five animals bearing squamous-cell carcinoma, in one of three dogs displaying mammary adenocarcinoma, and in the one dog that exhibited a transmissible venereal tumor. The results of this study support the additional evaluation of piroxicam in a phase II clinical trial in dogs bearing naturally occurring tumors.
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Patients were randomly assigned to receive parecoxib 80 mg daily i.v. (Group A), lornoxicam 16 mg daily i.v. (Group B) or diclofenac 150 mg daily i.m. (Group C). Rescue analgesia in all groups consisted of pethidine 25 mg i.m. Pain was measured with an analogue scale (pain intensity score).
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The actions of bradykinin on colonic epithelia from essential fatty acid-deficient (EFAD) rats has been examined. Electrogenic chloride secretion as short circuit current (SCC) and release of immunoreactive prostaglandin E2 (iPGE2) and i 6-keto PGF1 alpha have been measured. Resting release of prostanoids was significantly less in EFAD than in control tissues. Bradykinin, in a maximally effective concentration, produced no increase in prostanoid release in EFAD tissues in contrast to controls, while the SCC response was 55% of that in controls. In EFAD tissues the SCC response to bradykinin was the same whether or not the cyclooxygenase inhibitor piroxicam was present. EFAD tissues were not more sensitive to prostaglandins than control tissues. We conclude that while prostaglandin release contributes to the totality of the response to bradykinin, the latter's effect on electrogenic chloride secretion does not require the obligatory production of arachidonic acid metabolites.
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We compared the efficacy and tolerability of oral piroxicam 1 mg/kg/day with soluble aspirin given at 100 mg/kg/day taken four-hourly in 58 patients with sickle cell anaemia and severe ostcoarticular painful attacks requiring hospitalization in a randomized, paralleled study. Main investigational criteria were pain relief, limitation of movement, fever, and insomnia or agitation. Both groups were well-matched at the commencement of therapy but most patients on piroxicam showed remarkable and significant pain relief and improvement in other parameters within 24 h. Unwanted effects were absent in the piroxicam-treated group whereas those treated with aspirin experienced nausea and vomiting. There were no significant changes in liver function tests with both forms of treatment. Oral piroxicam is an effective and safe treatment in the management of the osteoarticular painful crisis in sickle cell anaemia. It might prevent the use of parenteral analgesics and hospitalization and reduce the loss of school hours in patients who are being treated for bone pain crises that characterize sickle cell anaemia.
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Drugs were separately, orally once daily dosed to pregnant rats from day 8 to 21 (GD1=plug day). Doses were set at 0.3, 3.0 and 30.0mg/kg for piroxicam and 0.2, 2.0 and 20.0mg/kg for DFU. Fetuses were delivered on GD 21 and routinely examined. Comprehensive clinical and developmental measurements were done. The pooled statistical analysis for ventricular septal (VSD) and midline (MD) defects was performed for rat fetuses exposed to piroxicam, selective and non-selective COX-2 inhibitor based on present and historic data.